Abemaciclib
Abemaciclib, sold under the brand name Verzenio among others, is a medication for the treatment of advanced or metastatic breast cancers. It was developed by Eli Lilly and it acts as a CDK inhibitor selective for cyclin-dependent kinases CDK4 and CDK6.[1] See also Abemaciclib and CDK4. Like the related drugs palbociclib and ribociclib, abemaciclib inhibits the enzymes cyclin-dependent kinase 4 (CDK4) and cyclin-dependent kinase 6 (CDK6).[2] These enzymes are responsible for phosphorylating and thus deactivating the retinoblastoma protein, which plays a role in cell cycle progression from the G1 (first gap) to the S (synthesis) phase.[3] Blocking this pathway prevents cells from progressing to the S phase, thereby inducing apoptosis (cell death).[2] In vitro analysis using cancer cell lines, it is reported that abemaciclib induces non‐apoptotic cell death characterized by formation of cytoplasmic vacuoles derived from lysosomes. This result suggests that there may be a mechanism of action other than inhibition of a cyclin-dependent kinase.[4] The X-ray co-crystal structure of human CDK6 and Abemaciclib (5l2s). Abemaciclib binding site. Water molecule is shown as red sphere.
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